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M8-B hydrochloride

A Potent and Selective Blocker of TRPM8 Channel

Cat #: M-220
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 432.96
    Purity: >99%
    Effective concentration 10 nM - 10 µM.
    Structure
    Chemical name N-(2-aminoethyl)-N-[(3-methoxy-4 phenylmethoxyphenyl) methyl]thiophene-2 carboxamide;hydrochloride.
    Molecular formula C22H25ClN2O3S.
    CAS No.: 883976-12-3
    PubChem CID 69316632
    Activity M8-B hydrochloride is a potent and selective blocker of TRPM8 channel, inhibiting rat and human TRPM8 activation by cold, by icilin and by menthol with IC50 values of 7.8 nM, 26.9 nM and 64.3 nM, respectively, whilst having little or no effect on other TRP channels (IC50 > 20 μM)1.
    References-Activity
    1. Almeida, M.C. et al. (2012) J. Neurosci. 32, 2086.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at +4°C.
    Solubility Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs M8-B hydrochloride inhibits TRPM8 channels expressed in HEK-293 cells.
      Alomone Labs M8-B hydrochloride inhibits TRPM8 channels expressed in HEK-293 cells.
      Dose response curve of TRPM8 inhibition by M8-B hydrochloride (#M-220). Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of M8-B hydrochloride, and activated by 30 nM Icilin. Changes in intracellular Ca2+ following agonist application were detected as changes in 485nm/525nm fluorescence (RFU). IC50 was determined at 20 nM.
    References - Scientific background
    1. Almeida, M.C. et al. (2012) J. Neurosci. 32, 2086.
    2. Tsumura, M. et al. (2013) PLoS ONE  8, e82233.
    3. Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
    Scientific background

    M8-B hydrochloride is a potent and selective antagonist of the transient receptor potential melastatin-8 (TRPM8) channel1. It inhibits rat and human TRPM8 channels by cold, by icilin and by menthol and demonstrates IC50 values of 7.8 nM, 26.9 nM, and 64.3 nM, respectively. The compound shows little or no effect on other TRP channels1.

    TRPM8 is a Ca2+-permeable channel, a member of the ‘long' or melastatin (M) group of TRP channels and is activated by temperatures range of 8–28°C or by cooling compounds. The TRPM8 gene is up-regulated in prostate cancer and other malignancies. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons2,3.

    Target TRPM8 channel
    Lyophilized Powder
    Last update: 06/11/2022

    M8-B hydrochloride (#M-220) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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